It has been recognized for many years that the mammalian body requires for its nutrition relatively large amounts of fats, carbohydrates and proteins, and by contrast relatively small amounts of vitamins and minerals; lack of these latter classes of substances has been held to be accountable for the absence of general good health as well as the incidence of various specific bodily ailments. Vitamins and minerals are normally ingested or otherwise produced from the mammalian diet, but to a certain extent may also or alternatively be produced in the body. For various reasons which may be related to the source of supply or the manufacturing processes used, foods are sometimes lacking or deficient in vitamins and/or minerals, and even where vitamins are synthesized in the body, such a process may not produce the amount required. Over a period of time there has therefore grown up the use of food supplements, to supply the ingredients of this nature required by the body, but which are either no produced therein in sufficient amounts, or are not supplied thereto by the regular diet of the subject in sufficient amounts.
Food supplements are not at the present time, however, restricted merely to a content of vitamins and minerals, as the sole active ingredients. Other materials which are intermediate in metabolic processes and which it is thought may not be produced i sufficient amounts (at least in subjects with abnormal metabolism) may also be present in food supplements. Examples of such other materials are unsaturated fatty acids, such as linoleic acid, gamma-linolenic acid, dihomo-gamma-linolenic acid arachidonic and eicosapentaenoic acids, as well as physiologically compatible derivatives thereof, such as salts, esters and amides of such acids, which may be metabolized in the body to prostaglandins. Prostaglandins are an important group of local hormones which act within the body tissues in which they are synthesized, in roles which are not entirely understood, though they may act at least to lower blood pressure, and to induce smooth muscle to contract.
Horrobin, in Med. Hypotheses 6: 469-486 (1980), has also proposed that a metabolic abnormality in the synthesis of certain prostaglandins is responsible for allowing an initial cancer cell to divide indefinitely, the abnormality being in particular, inhibition of the enzyme delta-6-desaturase which converts essential unsaturated fatty acids in normal cells to prostaglandins. He has also proposed pharmaceutical compositions (see e.g. EP No. 0037175 published Oct. 7, 1981 and prior patent applications referred to therein, the contents of which are to be regarded as incorporated herein by reference) comprising certain unsaturated fatty acids together with other ingredients which enhance formation in the body of essential prostaglandins and therefore bypass the metabolic abnormality referred to above.
Vitamin E is known to protect red blood cells, vitamin A and unsaturated fatty acids from oxidation, and to possess an important function in muscle maintenance. The possible influence of vitamin E on fertility is not regarded as having been proved, at least so far as humans are concerned. Ames, in Science 221: 1256-64 (1983), has suggested that certain mutagens and carcinogens in the diet may act through the generation of oxygen radicals, which may also play a role in the initiation of degenerative processes possibly related to cancer, heart disease and aging, and that dietary intake of natural antioxidants (many of which are identified as anticarcinogenic) could be an important aspect of the body's defense mechanism against such agents. Ames brings references to show that vitamin E is the major radical trap in lipid membranes, has been used clinically in a variety of oxidation-related diseases, ameliorates both the cardiac damage and carcinogenicity of adriamycin and daunomycin, protects against radiation-induced DNA damage, and increases the endurance of rats during heavy exercise. It is of interest that carotenoids such as beta-carotene, as well as ascorbic acid (vitamin C), are also mentioned by Ames as examples of a small number of other substances having both antioxidant and anticarcinogenic activity.
The present inventors have discovered that certain substances extracted from plants, as will be described hereinbelow, have antioxidant properties believed to be superior to those of the synthetic antioxidants butylated hydroxy anisole (BHA) and butylated hydroxy toluene (BHT).
Moreover, the inventors have also discovered that not only are the antioxidant properties of these plant-extracted substances apparently superior to those of vitamin E, but that similarly to vitamin E they improve the synthesis in vivo of prostaglandins, and that furthermore, they have antiaging and anticancer properties.
Vitamin E capsules and other liquid and solid preparations are listed (e.g.) in the U.S.P., and proprietary preparations are also available. The Physicians' Desk Reference (1982), publ. Medical Economics Co. Inc., Oradell, N.J., U.S.A. lists some 34 proprietary multivitamin preparations containing vitamin E, For a description of human requirements and uses of vitamin E, reference may be made Martindale, The Extra Pharmacapoeia, e.g. 28th Edition (1982) at page 1663 et seq. It is of interest in relation to the foregoing discussion that it has been recommended that at least 0.4 mg. alphatocopherol be administered for each gram of polyunsaturated acids. The relevant contents of these various publications are to be regarded as incorporated herein by reference. It is believed that the experiments carried out by the present inventors and described herein show that it should be possible to advantageously replace vitamin E where currently used by the water-soluble antioxidant materials defined in the present invention.
It is accordingly an object of the present invention to produce antioxidant plant extracts which may be used in place of vitamin E in food supplements.
It is also an object of the invention to use such antioxidant plant extracts in food supplements either alone or together with one or more vitamins and/or minerals and/or unsaturated fatty acids.
It is a further object of the invention to use such antioxidant plant extracts together with one or more unsaturated fatty acids known to be intermediates in the metabolic formation of prostaglandins in the mammalian body, with or without other ingredients which are known to enhance formation in the body of essential prostaglandins.
Other objects of the invention will appear from the description of the invention which follows.
The stable, water soluble plant-extracted antioxidants which constitute an essential ingredient of the present food supplements, and certain uses of these antioxidants, are described and claimed in U.S. Pat. Application Ser. No. 846,599, filed Mar. 31, 1986, now U.S. Pat. No. 4,857,325 (a continuation-in-part from Application Ser. No. 726,540, filed Apr. 24, 1985 as well as in European Patent Application No. 201,956 published November 1986.